Sunitinib Malate

Licensed by Pfizer Catalog No.S1042

Sunitinib Malate Chemical Structure

Molecular Weight(MW): 532.56

Sunitinib Malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit.

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In DMSO USD 191 In stock
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USD 147 In stock
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Cited by 42 Publications

12 Customer Reviews

  • PDGF-AA induces Ezh2 expression and proliferation in juvenile islets but not in adult islets. Western immunoblots of indicated islet proteins from 3 week or 9 month-old WT islets 2 days after exposure to PDGF-AA alone, or PDGF-AA plus RTK inhibitors Sunitinib.

    Nature 2011 478(7369):349-55. Sunitinib Malate purchased from Selleck.

    Assessment of effects on human juvenile or adult islets after exposure to PDGF-AA (50 ng/ml) for 2 days, with or without Sunitinib (2 uM) or U0126 (10 uM)co-treatment. Average percentage of BrdU+ insulin+ cells was morphometry from sectioned islets immunostained for insulin (green), glucagon (white) and BrdU (red). n = 3-6 independent experiments.

    Nature 2011 478(7369):349-55. Sunitinib Malate purchased from Selleck.

  • Combinational treatment of kinase inhibitors induces the similar phenotype produced by PP1. All images are lateral view with dorsal to the top and anterior to the left. The combinational treatment of Dasatinib (D) or U0126 (U) with Sunitinib (SU),PTK787 (PTK), or ZM323881 (Z) resulted in the shrinkage of dorsal aorta.

    Cell Res 2011 21, 1080-1087. Sunitinib Malate purchased from Selleck.

    A, Tumor growth curves from the initial sunitinib drug trials, with endpoint set at 1,300 mm3 (mean ± SEM). Measurements began one week after tumor inoculation and on the day sunitinib treatment began. Subsequent experimental endpoints were set on the basis of these growth curves and their intersections with this data are shown. B, Histogram plot showing the distribution of tumor sizes at day 8 of treatment. Sunitinib-treated tumors exceeding 250 mm3 in size were identified as falling into the nonresponsive cohort. Sunitinib treatment significantly retards growth of responsive tumors.

    Cancer Res, 2017, 77(4):1008-1020 . Sunitinib Malate purchased from Selleck.

  • Sunitinib decreases FLT-3 and RET phosphor ylation but increases ERK phosphorylation in a time-dependent manner. H295R and SW13 cells were treated with sunitinib (10 nM) for various time points as indi-cated. Cell lysates were prepared and phospho-FLT-3, RET, and ERK levels were monitored by Western Blot-ting. Re-probing against FLT-3, RET, and ERK was done to ensure equal protein loading.

    Surgery 2012 152, 1045-50. Sunitinib Malate purchased from Selleck.

    Sunitinib or PD98059 decreases cell proliferation in a dose-dependent manner. H295R and SW13 cells were treated with various concentration of sunitinib or PD98059 for 48 hours as indicated. Treated cells were subjected to the MTS proliferation assay. Similar experiments were repeated 3 times. Histograms represent relative % of OD490 nm absorbance (* P < .05). All data are relative multiples of expression compared with untreated cells. The data are representative of three experiments and are expressed as the mean ?SE.

    Surgery 2012 152, 1045-50. Sunitinib Malate purchased from Selleck.

  • Autophagic activation in sunitinib- and sorafenib- but not AZD6244-treated cells. Medullary thyroid cancer-1.1 (MTC-1.1; A) and TT ( B) cells were treated with dimethyl sulfoxide (DMSO), sunitinib (50 nM), sorafenib (10 nM), AZD6244 (30 nM), or everolimus (20 nM) for 48 hours. Cell lysates were prepared, and light chain 3 (LC3)-I and -II cleaved caspase-3 protein levels were monitored by Western blotting. Reprobing against actin was per formed to ensure equal protein loading. ( C ) MTC-1.1 and TT cells were transiently transfected with autophagy protein 5 (Atg-5) small inter fering RNA. Transfection with scrambled small inter fering RNA was used as a control. After transfection, cells with and without Atg-5 knockdown were exposed to DMSO or 20 nM of everolimus for 48 hours. Cell lysates were pre- pared and LC3-I and -II protein expression levels were monitored by Western blotting. Reprobing against Atg-5 was per formed to monitor Atg-5 knockdown efficiency. Reprobing against actin was per formed to ensure equal protein.

    Surgery 2012 152, 1142-9. Sunitinib Malate purchased from Selleck.

    Autophagy inhibition blocks the antiproliferative effects of sunitinib and sorafenib but not AZD6244. Medullary thyroid cancer–1.1 (MTC-1.1) and TT cells were transfected transiently with scrambled or autophagy protein 5 (Atg-5) small inter fering RNA. After transfection, cells with and without Atg-5 knockdown were exposed to sunitinib (50 nM), sorafenib (10 nM), and AZD6244 (30 nM) for 48 hours. Treated cells were subjected to a 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium proliferation assay. Similar experiments were repeated 3 times. Histograms represent the relative percent of OD490 nM absorbance. The asterisk indicates significance versus scrambled small inter fering RNA–treated control ( P < .05). All data are relative multiples of expression compared to untreated cells. The data are representative of 3 experiments and are expressed as the mean ± the standard error.

    Surgery 2012 152, 1142-9. Sunitinib Malate purchased from Selleck.

  • Sunitinib limits the colonial growth of HT-29 by downregulating HIF-1a. (A) The number and size of colonies formed in soft agar. The numbers of small colonies (<50 μm diameter) were not different among conditions of a serial concentration of sunitinib. On the contrary, large colonies (>50 μm diameter) disappeared after incubation with sunitinib. Each point represents the mean and SD from four separate experiments. (B) HIF-1a expression and hypoxia within HT-29 colony. After colonies grew for 4 weeks, HIF-1a and hypoxia were visualized by immunofluoroscence staining. Bar = 20 μm.

    Biochem Bioph Res Co 2010 398, 205–211. Sunitinib Malate purchased from Selleck.

    2. Sunitinib downregulates HIF-1a. (A) Dose-dependent repression of HIF-1a protein level by sunitinib in HT-29. HT-29 cells were incubated under normoxic (N) or hypoxic (H) conditions in the presence of sunitinib for 24 h. HIF-1a and ARNT proteins in total cell lysates were analyzed by Western blotting. (B) Sunitinib attenuates the hypoxic induction of HIF-1 target genes. RNAs were isolated from HT-29 cells subjected to normoxia (N) or hypoxia (H) in the presence of sunitinib for 16 h. The mRNAs of HIF-1a and its target genes were analyzed by RT-PCR and autoradiography. PGK1 indicates phosphoglycerate kinase 1; PDK1, pyruvate dyhydrogenase kinase 1; CAIX, carbonic anhydrase IX. (C) Sunitinib-induced HIF-1 inhibition. Epo-enhancer and b- galactosidase reporter plasmids were co-transfected into HEK293 cells. After 16 h incubation, luciferase and b-galactosidase activities were measured. *P < .05 versus the hypoxic control.

     

     

    Biochem Bioph Res Co 2010 398, 205–211. Sunitinib Malate purchased from Selleck.

  • Sunitinib inhibits 50-UTR-dependent translation of HIF-1a. (A) 50 cap-dependent translational activity of HIF-1a. The luciferase reporter plasmid contains the HIF-1a 50-UTR segment between the tk promoter and the luciferase gene. HT-29 cells were co-transfected with the reporter plasmid (8 lg per 100-mm dish) and the b-gal plasmid (4 μg). After 16 h incubation under normoxic or hypoxic conditions with sunitinib, cells were lysed and subjected to luciferase assay. *P < .05 versus the hypoxic control. (B) IRES-dependent translational activity of HIF-1a. The luciferase reporter plasmid contains the HIF-1a 50-UTR segment between the GFP gene and the luciferase gene. HT-29 cells were co-transfected with the reporter plasmid (8 μg) and the b-gal plasmid (4 μg). *P < .05 versus the hypoxic control. (C) Sunitinib inhibits phosphorylation of Akt. After 8 h incubation under hypoxic condition with sunitinib, HT-29 cells were lysed and subjected to Western blotting. (D) Sunitinib suppresses HIF-1a in VHL-null RCC4 cells. VHL (-/-) RCC4 cells were incubated under normoxic conditions sunitinib for 8 h, and HIF-1a in total cell lysates was analyzed by Western blotting.

     

     

    Biochem Bioph Res Co 2010 398, 205–211. Sunitinib Malate purchased from Selleck.

    Experimental layout for VEGF signaling blocking and LCMV infection in WT mice. Mice received two injections on day 0 and 3 p.i. of Abs as described in Material and Methods, or daily gavage of the VEGFR/PDGFR-inhibitor sunitinib. Inguinal LN volume on day 0 (D0) or day 8 (D8) p.i. after treatment of mice with control Ig or anti-VEGFR2, anti-VEGF-A Abs or sunitinib. Pooled from 1-2 independent experiments with 3-5 mice per treatment. D. Total HEV length on day 0 (D0) or day 8 (D8) p.i. as in C. No significant difference was found in C and D between day 8 control Ig and Ab- or inhibitor-treated values (One-way ANOVA).

    AACR Sunitinib Malate purchased from Selleck.

Purity & Quality Control

Choose Selective PDGFR Inhibitors

Biological Activity

Description Sunitinib Malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit.
Targets
Kit [1]
(Cell-free assay)
FLT3 [1]
(Cell-free assay)
PDGFRβ [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
2 nM 80 nM
In vitro

Sunitinib also potently inhibits Kit and FLT-3. [1] Sunitinib is a potent ATP-competitive inhibitor of VEGFR2 (Flk1) and PDGFRβ with Ki of 9 nM and 8 nM, respectively, displaying >10-fold higher selectivity for VEGFR2 and PDGFR than FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl, and src. In serum-starved NIH-3T3 cells expressing VEGFR2 or PDGFRβ, Sunitinib inhibits VEGF-dependent VEGFR2 phosphorylation and PDGF-dependent PDGFRβ phosphorylation with IC50 of 10 nM and 10 nM, respectively. Sunitinib inhibits VEGF-induced proliferation of serum-starved HUVECs with IC50 of 40 nM, and inhibits PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFRβ or PDGFRα with IC50 of 39 nM and 69 nM, respectively. [2] Sunitinib inhibits phosphorylation of wild-type FLT3, FLT3-ITD, and FLT3-Asp835 with IC50 of 250 nM, 50 nM, and 30 nM, respectively. Sunitinib inhibits the proliferation of MV4;11 and OC1-AML5 cells with IC50 of 8 nM and 14 nM, respectively, and induces apoptosis in a dose-dependent manner. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
3T3 NFrBZoNMcW6jc3WgRZN{[Xl? NFXyS3BKdmirYnn0bY9vKG:oIGDES2YucW6mdXPl[EBDemSXIHnuZ49zeG:{YYTpc44hf2m2aDDJR|UxKG:oIECuNFA4KM7:TR?= NGXuO2EyOjZ2NkCxPS=>
3T3 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\HXGlvcGmkaYTpc44hd2ZiUHzheIVt\XRvZHXybZZm\CCpcn;3eIgh\mGldH;yJIlv\HWlZXSgN3Q{KGOnbHygdJJwdGmoZYLheIlwdiC5aYToJGlEPTBib3[gNE4xOSEQvF2= NXnzZVg3OTJ4NE[wNVk>
3T3 MXPGeY5kfGmxbjDBd5NigQ>? MoTiTY5pcWKrdHnvckBw\iCYYYPjeYxieiCnbnTveIhmdGmjbDDndo94fGhiZnHjeI9zKHKnY3XweI9zKHerdHigTWM2OCCxZjCwMlA2KM7:TR?= NFe4cYkyOjZ2NkCxPS=>
3T3 NGDqSlVMcW6jc3WgRZN{[Xl? NV\UcG16OjBibXnu MofxSG1UVw>? M3HOcmNmdGy3bHHyJIlvcGmkaYTpc44hd2ZiVlXHSkBqdmS3Y3XkJIh2dWGwIFvEVkBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEKyJO69VQ>? NV7RV3JQOTZzNkKwNFg>
NIH3T3 MXnLbY5ie2ViQYPzZZk> MmXmNlAhdWmw M12y[mROW09? MmiwbY5pcWKrdDDoeY1idiCNRGKgb4lv[XOnIHX4dJJme3OnZDD3bZRpKEmFNUCgc4YhOC5yMUig{txO M2H2XlE3OTZ{MEC4
A549 NE\wSIpHfW6ldHnvckBCe3OjeR?= NI[1T3hFVVOR MnHNTY5pcWKrdHnvckBw\iClLV3leEBl\XCnbnTlcpQhUEeILXnu[JVk\WRiaIXtZY4hSTV2OTDj[YxtKG2rZ4LheIlwdiC5aYToJGlEPTBib3[gNkDPxE1? MX[xPFQ{PDF2NR?=
DU145 MXvGeY5kfGmxbjDBd5NigQ>? MYPEUXNQ M2jIV2lvcGmkaYTpc44hd2ZiYz3N[ZQh\GWyZX7k[Y51KEiJRj3pcoR2[2WmIHj1cYFvKESXMUS1JINmdGxic3PheJRmemmwZzD3bZRpKEmFNUCgc4YhOTBizszN MUexPFQ{PDF2NR?=
KB3-1 NYfnVVJnS3m2b4TvfIlkKEG|c3H5 NH\E[VQ4OiCq M37peWROW09? NGXLWZFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRNWeyLX7l[4F1cX[nIFvCMVMuOSClZXzsd{B4cXSqIFnDOVAhd2ZiMj6zJO69VQ>? NYTZO2pvOTl|OUezNlI>
KBV1 MWjDfZRwfG:6aXOgRZN{[Xl? NEL3R|U4OiCq MVTEUXNQ MYHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQMYdtgWOxcILveIVqdi2neIDy[ZN{cW6pIFvCWlEh[2WubIOge4l1cCCLQ{WwJI9nKDRwMTFOwG0> MY[xPVM6PzN{Mh?=
A375 NX\jWZFmS3m2b4TvfIlkKEG|c3H5 NEnoRW04OiCq NUDNU4J5TE2VTx?= NITR[o5KSzVyPUWuOEDPxE1? MVuxPVY2PDRyOB?=
RS4-11 NYXPZVdNTnWwY4Tpc44hSXO|YYm= Ml:5NkBp NIrGZ2hKdmirYnn0bY9vKG:oIF\MWFMh[XW2b4Doc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4xODl7IN88US=> Mke0NVk3PTR2MEi=
RS4-11 MnzDSpVv[3Srb36gRZN{[Xl? MnntNkBp NV7TdVBzUW6qaXLpeIlwdiCxZjDGUHQ{KEmWRDDteZRidnRiYYX0c5Bpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yM{Sg{txO NI\ZT2QyQTZ3NESwPC=>
Sf9 MWnLbY5ie2ViQYPzZZk> MXKzNEBucW5? MXXJcohq[mm2aX;uJI9nKEeVVD30ZYdo\WRiVlXHSnIh\XiycnXzd4VlKHerdHigTWM2OCCxZjCwMlE5PSEQvF2= NIPxXmMyQTh3NEC1NS=>
Ba/F3 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUG3NkBp NYKxTXlVUUN3ME2xMlIh|ryP M4n2S|IxOTF5MEC0
BaPTC2 Ml\GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\MSoc4OiCq NInEXVdKSzVyPUCuNlIh|ryP M2DPb|IxOTF5MEC0
Sf9 NXLjU2JRTnWwY4Tpc44hSXO|YYm= MVWxJIg> Mk\lSG1UVw>? MVTJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KEircz30ZYdo\WRiUlXUJIV5eHKnc4Pl[EB4cXSqIFnDOVAhd2ZiMT6zJO69VQ>? M363fFIxOTF5MEC0
H4 NH6zc|hEgXSxdH;4bYMhSXO|YYm= M{LKNVExKM7:TR?= NV:ybVZQXG:6aXPpeJkhcW5iaIXtZY4hUDRiY3XscJM> NVHObHFROjB|NUC4NFY>
SF-539 NHj0fpBMcW6jc3WgRZN{[Xl? MWCzN|Mh|ryP MWW2NEBucW5? M3TvdmROW09? MmDOTY5pcWKrdHnvckBw\iCSRFfGVoJmfGFicHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCxNk4zKM7:TR?= MnPxNlA1ODN5MEC=
U251 NFvlOmdMcW6jc3WgRZN{[Xl? MmHjN|M{KM7:TR?= MVy2NEBucW5? NHTsbnVFVVOR NITucFRKdmirYnn0bY9vKG:oIG\FS2ZTOiCyaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIEG4Mlkh|ryP NHH3VpUzODRyM{ewNC=>
A431 NFX5eIFMcW6jc3WgRZN{[Xl? NUe2UHYzUW6qaXLpeIlwdiCxZjDQSGdHWmKndHGg[ZhxemW|c3XkJJdqfGhiSVO1NEBw\iBzMj6yJO69VQ>? NIDtWJozODV3OEC3Ni=>
A431 NH\scpVMcW6jc3WgRZN{[Xl? NU[2e5FpUW6qaXLpeIlwdiCxZjDWSWdHWjJiZYjwdoV{e2WmIIfpeIghUUN3MDDv[kAyQC57IN88US=> Ml:4NlA2PThyN{K=
HepG2 NIH6WFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHEO|IhcA>? MkDKTWM2OD1|LkixJO69VQ>? NYLmcWR4OjB3N{C1NlY>
Kasumi-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInsXo44OiCq M4roTGlEPTB;MD6wNVYh|ryP NHnvcJkzODV5MEWyOi=>
RS4-11 NFHwNmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVS3eYxIPzJiaB?= NI\lbYlKSzVyPUGg{txO NIGwN3AzODV5MEWyOi=>
THP1 MlLiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXsfZF[PzJiaB?= MlPLTWM2OD1yLkWg{txO MVGyNFU4ODV{Nh?=
Kasumi-1 NYrPdJZtTnWwY4Tpc44hSXO|YYm= M33lSGlvcGmkaYTpc44hd2ZiYz3LbZQh[XW2b4Doc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4xOTVizszN M{HRUVIxQDN|MEO5
A549 NGHlOplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUixOkBp NVLzdYRRSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsdy=> M4HiWVIyPDVyNE[z
HL60 M4H3emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTTNI8yOTZiaB?= MUDBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTE[wJINmdGy| MWiyNVQ2ODR4Mx?=
HUVEC NGTFWpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF:zbnIyPiCq M4LGW2lvcGmkaYTpc44hd2ZiVlXHSk1qdmS3Y3XkJINmdGxicILvcIln\XKjdHnvckB4cXSqIFnDOVAhd2ZiMj63OUDPxE1? NYDKWHIyOjF2NUC0OlM>
HUVEC NGX6dHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfIWWgyPiCq M1;jUGlvcGmkaYTpc44hd2ZiYl\HSk1qdmS3Y3XkJINmdGxicILvcIln\XKjdHnvckB4cXSqIFnDOVAhd2ZiND6wOEDPxE1? M3[0UFIyPDVyNE[z
IM9 NYXxeVFnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\WeVE3KGh? MXzBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCLTUmgZ4VtdHN? NVLLXZNGOjF2NUC0OlM>
K562 NGnQdXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vFOFE3KGh? MmS3RY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS{W2NkBk\Wyucx?= MU[yNVQ2ODR4Mx?=
MDA-MB-231 NV3RdodpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHLNVYhcA>? MojoRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[Yxtew>? M4D0ZVIyPDVyNE[z
H460 Mk\PR5l1d3SxeHnjJGF{e2G7 M2nMOFczKGh? Mn3sTWM2OD1{Lkeg{txO Mn;NNlE3OjF6OEC=
SMMC7721 NIfHTphEgXSxdH;4bYMhSXO|YYm= M3vnbFczKGh? NIPqOoRKSzVyPU[uOFch|ryP M1jMe|IyPjJzOEiw
WI38 M{js[GN6fG:2b4jpZ{BCe3OjeR?= M4K2U|czKGh? Mn\uTWM2OD16LkW2JO69VQ>? NVi5[4ZxOjF4MkG4PFA>
HEK293 NX3xRoNEU2mwYYPlJGF{e2G7 MkntNVAxKG6P MmflNUBp NH3CSopld2W|IH7veEBqdmirYnn0JHZGT0ZvaX7keYNm\CCjdYTvdIhwe3Cqb4L5cIF1cW:wIH;mJJR6em:|aX7lJFEyPzVicnXzbYR2\SCxbjDWSWdHWjJiZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[Yxtew>? NFTyWHYzOTh6NUK4Oy=>
HUVEC NFvNOGFHfW6ldHnvckBCe3OjeR?= NGTBOWoyKM7:TR?= NF7kfWYzPCCq NFPvfGFCdnSrYX7nbY9o\W6rYzDhZ5Rqfmm2eTDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCYRVfGMYlv\HWlZXSgZ4VtdCCvaXfyZZRqd25? Ml[yNlE6PjN|MEW=
HUVEC NISycJlHfW6ldHnvckBCe3OjeR?= NES1OXAyKM7:TR?= NXW4WnRVOSCq MlvwTY5pcWKrdHnvckBw\iCHUlugdIhwe3Cqb4L5cIF1cW:wIHH0JHRpejJyMj;UfZIzODRiaX6gWmVITi2|dHnteYxifGWmIFjVWmVE NV71UnBGOjF7NkOzNFU>
HUVEC NXi4dG1kTnWwY4Tpc44hSXO|YYm= M{fze|Eh|ryP MXmxJIg> M4WyTWlvcGmkaYTpc44hd2ZiZV7PV{BxcG:|cHjvdplt[XSrb36gZZQhW2W{LUGxO|IhcW5iVlXHSk1{fGmvdXzheIVlKEiXVlXD NV;QXnJuOjF7NkOzNFU>
HUVEC M4rUXGtqdmG|ZTDBd5NigQ>? MYOxJO69VQ>? MnjLNUBp NFG5N3VKdmirYnn0bY9vKG:oIG\FS2ZTOiCyaH;zdIhwenmuYYTpc44h[XRidInyMVEyPzViaX6gWmVITi2|dHnteYxifGWmIFjVWmVE NVjPRpFwOjF7NkOzNFU>
HUVEC MYXGeY5kfGmxbjDBd5NigQ>? M3rPT|Eh|ryP M3jme|EhcA>? M1;6N4Rw\XNibn;0JIlvcGmkaYSgRWtVKHCqb4PwbI9zgWyjdHnvckBifCCVZYKtOFc{KGmwIG\FS2Yue3SrbYXsZZRm\CCKVW\FRy=> MYOyNVk3OzNyNR?=
HL60 MVHDfZRwfG:6aXOgRZN{[Xl? M2XDV|UxKM7:TR?= M{XVV|Q5KGh? NIWwTpNFVVOR MnfMTWM2OD1zNT61JO69VQ>? NV[4WHZMOjJyMUmxPFg>
K562 NH3zV5FEgXSxdH;4bYMhSXO|YYm= M1WydlUxKM7:TR?= M3z1dVQ5KGh? NULwO5BKTE2VTx?= MojRTWM2OD1{MT65JO69VQ>? MnX2NlIxOTlzOEi=
PC3 NEDGVGNEgXSxdH;4bYMhSXO|YYm= MnPzOVAh|ryP NX[5O5ZuPDhiaB?= NXXV[WdpTE2VTx?= NFPnPVdKSzVyPUK1MlEh|ryP MnXZNlIxOTlzOEi=
SF-539 MXnLbY5ie2ViQYPzZZk> MYezN|Mh|ryP M3\QRVYxKG2rbh?= MVnJcohq[mm2aX;uJI9nKFCGR1\SZoV1[SC2eYLvd4lv\SCtaX7hd4Uh[WO2aY\peJkhcW5iUFTHSk1DSi2|dHnteYxifGWmIHj1cYFvKFOILUWzPUBk\WyuczD3bZRpKEmFNUCgc4YhOTJwMjFOwG0> MoLONlIzODR5NEG=
HAEC NV3SclR6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vKflExOCEQvF2= NInRVJU4OiCq MoLkRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQVXDJINmdGy|IHX4dJJme3OrbnegWmVITlJid3n0bEBKSzVyIH;mJFAvOSEQvF2= NYLlSoZIOjJ2NES2O|k>
HT-29 MmCzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUexNFAh|ryP NWrMbnVnPzJiaB?= NF7iPXlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjUMVI6KGOnbHzzJIV5eHKnc4PpcochXkWJRmKge4l1cCCLQ{WwJI9nKDBwM{Og{txO NIHTVIMzOjR2NE[3PS=>
MV4-11 MXHDfZRwfG:6aXOgRZN{[Xl? M33yWVczKGh? M3vJV2lEPTB;MD6wNFMh|ryP M3XB[lIzPDV{NUG4
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PC9 NXHwZ3h{S3m2b4TvfIlkKEG|c3H5 MYC0PEBp MoC0TWM2OD1zMD65O{DPxE1? MWWyNlQ5OzZyOB?=
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SNB19 NEH3[IFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTaR44yODBizszN NIHxV5g1QCCq NYTmPIhxTE2VTx?= NWLNUFR2T0l3NE2xNEDPxE1? NEXFUIczOjV4ME[yOy=>
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UACC257 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\4R|ExOCEQvF2= NEXWWms1QCCq NVPjdVRuTE2VTx?= MUXHTVU4RTRizszN Mo[wNlI2PjB4Mke=
HAEC NF64[IxEgXSxdH;4bYMhSXO|YYm= NFjtXWwyODBizszN M2nx[lczKGh? NWL2fFBxTE2VTx?= MYPDfZRwfG:6aXPpeJkh[WejaX7zeEBXTUeIUjDlfJBz\XO|aX7nJGhCTUNid3n0bEBKSzVyIH;mJFAvOSEQvF2= NVLwTnJDOjNzM{G1OFE>
HT-29 M1:5UGN6fG:2b4jpZ{BCe3OjeR?= M3nJd|ExOCEQvF2= M1\JcFczKGh? M3LlVWROW09? Ml7WR5l1d3SxeHnjbZR6KGGpYXnud5QhXkWJRmKg[ZhxemW|c3nu[{BpfW2jbjDIWE0zQSClZXzsd{B4cXSqIFnDOVAhd2ZiMD6zN{DPxE1? M3nJdFI{OTNzNUSx
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ACHN NH;jdHlEgXSxdH;4bYMhSXO|YYm= MX[2JIQ> MnLxTWM2OD1{LkWg{txO MoP4NlM{PjBzMES=
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HUVEC NG\HNJZMcW6jc3WgRZN{[Xl? MmHxNlAxKM7:TR?= NYryNGQ4TE2VTx?= MYHJcohq[mm2aX;uJI9nKF[HR1\SNkBxcG:|cHjvdplt[XSrb36gbY4h\3Kxd4ToJIZi[3Sxcj3zeIlufWyjdHXkJGhWXkWF NWXkfJBuOjN3OEO5NVE>
HUVEC NHznV4xMcW6jc3WgRZN{[Xl? MWSyNFAh|ryP NF63NY9FVVOR NH7ZdllKdmirYnn0bY9vKG:oIG\FS2ZTOSCyaH;zdIhwenmuYYTpc44hcW5iZ4Lve5RpKG[jY4Tvdk1{fGmvdXzheIVlKEiXVlXD MWGyN|U5OzlzMR?=
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BGC M3Sze2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXq3NkBp MnntSG1UVw>? Mn7UTWM2OD12Lke4JO69VQ>? MVuyN|k6QTB2MB?=
BxPC3 NFriWIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUO3NkBp M{DrVmROW09? MnvRTWM2OD1|Lk[zJO69VQ>? NHX0Wo4zOzl7OUC0NC=>
HT-29 NEn6[GJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPZdow4OiCq NFrZOpZFVVOR M2jpTmlEPTB;MT60O{DPxE1? NIXkU40zOzl7OUC0NC=>
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MCF7 NHTNZZVEgXSxdH;4bYMhSXO|YYm= MUS3NkBp MYnEUXNQ NIfMWHlKSzVyPUCuNFI6OyEQvF2= MnjRNlQ5QTB4NUK=
MDA-MB-231 NI[zTndEgXSxdH;4bYMhSXO|YYm= MkPyO|IhcA>? MkKxSG1UVw>? NUTKTG81UUN3ME2wMlAzOjNizszN MXiyOFg6ODZ3Mh?=
MDA-MB-435 NGTGOpFEgXSxdH;4bYMhSXO|YYm= M2LBflczKGh? M1rtSGROW09? MXvJR|UxRTBwMEC5O{DPxE1? MYiyOFg6ODZ3Mh?=
MDA-MB-468 MUHDfZRwfG:6aXOgRZN{[Xl? MorDO|IhcA>? MV7EUXNQ NY\oR|MzUUN3ME2wMlAxPjFizszN MmnrNlQ5QTB4NUK=
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SH-SY5Y MYDLbY5ie2ViQYPzZZk> Ml3JNVAh|ryP MoL4NUBp NFv3ToFFVVOR NIjaVm9KdmirYnn0bY9vKG:oIGDES2ZT[mW2YTD3bZRpKEmFNUCgc4YhOC5yOEOxJO69VQ>? NIflbmQzPDh7ME[1Ni=>
U251 MoG2T4lv[XOnIFHzd4F6 NWq3eVFHOTBizszN MW[xJIg> NYXtToF7TE2VTx?= NHu0SY5KdmirYnn0bY9vKG:oIG\FS2ZTOiC5aYToJGlEPTBib3[gNE4xOTh7IN88US=> M{XC[|I1QDlyNkWy
Bel7402 MkDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXmyNFJ1PzJiaB?= NELsUYRFVVOR MljrTWM2OD1{Lk[3JO69VQ>? MXuyOFkxPDl4MR?=
HK2 M1fJfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4O5WVczKGh? Ml\SSG1UVw>? NGfLXHJKSzVyPUWuPFUh|ryP M1fkN|I1QTB2OU[x
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MV4-11 M2POdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELkXmE1QCCq NHe3UYNFVVOR M4riUGlEPTB;MD6wNFMh|ryP NF7vdWkzPDlyNEm2NS=>
NCI-H3122 Mn[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXi3NkBp M33LTmROW09? NUXuNWdDUUN3ME2wMlg{KM7:TR?= MkTLNlQ6ODR7NkG=
NCI-H460 M2XKOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVS3NkBp Mk\iSG1UVw>? MWrJR|UxRTRwM{Gg{txO M{PFRVI1QTB2OU[x
NCI-H526 Mm\TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYW3NkBp MX7EUXNQ MUDJR|UxRTFwMEGg{txO M2\LT|I1QTB2OU[x
TT NUWyOplpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXy3NkBp NX\OcY5MTE2VTx?= NWroT4VCUUN3ME2wMlA1KM7:TR?= NIXlbmszPDlyNEm2NS=>
EoL-1-cell M3HWVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rpfGlEPTB;MT62OEBxVQ>? NEfoVYFUSU6JRWK=
MV-4-11 NH3F[ItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTJ5MjDwUS=> M4rU[HNCVkeHUh?=
NOS-1 M4q2N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnf6TWM2OD1zNT6zJI5O MW\TRW5ITVJ?
CGTH-W-1 NE\PR5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\qTWM2OD1|MD65OEBvVQ>? NEPUZlRUSU6JRWK=
MONO-MAC-6 Ml34S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTN|Lkigcm0> NFPJd4VUSU6JRWK=
ALL-PO MmHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDzW4p1UUN3ME23PU45QSCwTR?= MV3TRW5ITVJ?
NKM-1 M1[wW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXDTWM2OD17OD61NkBvVQ>? NX:2OId[W0GQR1XS
KM12 NGTMRpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDoTWM2OD1|NUCuNVQhdk1? MUTTRW5ITVJ?
TE-15 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XFTGlEPTB;NUC3MlYyKG6P MkPIV2FPT0WU
697 M2\6V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTZzND6yOUBvVQ>? MlvvV2FPT0WU
MOLT-16 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvUZ|ZKSzVyPU[zNU4{OiCwTR?= MXvTRW5ITVJ?
GB-1 M1Po[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV[xOJg3UUN3ME23NVAvOjNibl2= M2TkdnNCVkeHUh?=
TE-12 NV[2bmZyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TYZ2lEPTB;OEC0MlU2KG6P MXzTRW5ITVJ?
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LC-2-ad NVzWbFJIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTFwMUG0NFch|ryP MmDuV2FPT0WU
BL-70 MmHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnOOos3UUN3ME2xMlEyQDR4IN88US=> MYnTRW5ITVJ?
ETK-1 Mn7HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTFwMki1PEDPxE1? MkSwV2FPT0WU
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SIG-M5 M17IT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HXNmlEPTB;MT6zO|AxQSEQvF2= MVrTRW5ITVJ?
NCI-SNU-16 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTFwNE[0PFYh|ryP MnX5V2FPT0WU
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A3-KAW NIe4b2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjlcIpKSzVyPUGuOlI2PDZizszN M4nNTXNCVkeHUh?=
KS-1 M1vJSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\nc|JHUUN3ME2xMlY6OjR5IN88US=> NUDxRYp6W0GQR1XS
CTV-1 NUXUfJRWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrJc2dtUUN3ME2xMlczPzVzIN88US=> Ml\vV2FPT0WU
LB1047-RCC NIK2ZmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLTb|JKSzVyPUGuPFE3OjRizszN NUXjbo9vW0GQR1XS
EMG-01 NEfBd2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTFwOEO1OlMh|ryP M4LvdnNCVkeHUh?=
TE-11 NETGcGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHa[2xKSzVyPUGuPFM6QDVizszN NXGxXHBuW0GQR1XS
CMK MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvzPJU4UUN3ME2xMlk2PTF5IN88US=> NWq2b3JxW0GQR1XS
NB1 M{nRUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVi4WHppUUN3ME2xMlk3OTF5IN88US=> NYPRfXE3W0GQR1XS
HAL-01 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfFfFh[UUN3ME2yMlA2QTR4IN88US=> MX;TRW5ITVJ?
DEL M{\lcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmm4TWM2OD1{LkC4OFgzKM7:TR?= Mn76V2FPT0WU
RL95-2 MmTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXaTWM2OD1{LkGxNVM4KM7:TR?= MUPTRW5ITVJ?
KARPAS-299 M4fiWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\DVWRVUUN3ME2yMlEyOzF|IN88US=> MlO5V2FPT0WU
EW-16 NFK0TIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfQPWw1UUN3ME2yMlE{PTB6IN88US=> M1jvZnNCVkeHUh?=
RS4-11 M3XBOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfVdYJKSzVyPUKuNVc6OjRizszN NF\OOlFUSU6JRWK=
BB30-HNC MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLJTWM2OD1{LkKyN|c2KM7:TR?= MXnTRW5ITVJ?
DOHH-2 M1vp[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;rcYVKSzVyPUKuN|M1OzFizszN Mof4V2FPT0WU
RPMI-8402 M1;XUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTJwM{O2NVgh|ryP M2LTSXNCVkeHUh?=
BV-173 NV65TI84T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDVV49KSzVyPUKuN|M3PiEQvF2= NGLOSXhUSU6JRWK=
TE-10 NWfpXGFMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nvbmlEPTB;Mj6zOFM5PCEQvF2= NYfxfpZkW0GQR1XS
TE-8 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3ftfGlEPTB;Mj6zO|A{QCEQvF2= MnjxV2FPT0WU
K052 NGX1OGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPRUItUUUN3ME2yMlQxOjB{IN88US=> MXfTRW5ITVJ?
KARPAS-45 NIfxflBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7TTWM2OD1{LkS5OFQ3KM7:TR?= NFHFUHNUSU6JRWK=
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KGN NInwZlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTJwNkCzN|kh|ryP NHOyN5JUSU6JRWK=
ML-2 MlXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml73TWM2OD1{Lk[zOVEzKM7:TR?= MWnTRW5ITVJ?
LAMA-84 NYrzb2lMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jjWGlEPTB;Mj62PVU1PSEQvF2= NWS0fZRIW0GQR1XS
LXF-289 M{LVc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml[5TWM2OD1{LkeyPVg6KM7:TR?= M4LIfHNCVkeHUh?=
A101D M2XNVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nvXmlEPTB;Mj63PFMxPCEQvF2= M3yzUXNCVkeHUh?=
KY821 M{i5NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPsTWM2OD1{Lke5O|U5KM7:TR?= NFHycFJUSU6JRWK=
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MHH-PREB-1 M2DlWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTCPYdkUUN3ME21MlMzOzF{IN88US=> M1nXd3NCVkeHUh?=
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TALL-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRThwMUizPFQh|ryP NWXydHIzW0GQR1XS
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CI-1 NXjUSIVNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVmz[2hIUUN3ME24MlIxPDFzIN88US=> NFn3fo5USU6JRWK=
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OVCAR-4 MlXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRThwNUCzOVEh|ryP MYrTRW5ITVJ?
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NCCIT NY\0TokzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDNdJlZUUN3ME24MlcyPzR3IN88US=> MWHTRW5ITVJ?
NCI-H1648 NXf4TGdWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nGdGlEPTB;OT6xN|g{PCEQvF2= MWLTRW5ITVJ?
COR-L279 MlrXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fKUmlEPTB;OT6zPVA6KM7:TR?= MW\TRW5ITVJ?
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VA-ES-BJ MnXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonDTWM2OD17Lkm5PVM{KM7:TR?= MUTTRW5ITVJ?
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NCI-H128 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jKW2lEPTB;MUOuNFczOyEQvF2= M2n5UnNCVkeHUh?=
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KP-N-YS MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTF2LkK4PVQh|ryP M{D2eXNCVkeHUh?=
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NCI-H1770 NGnmbZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDMR3VNUUN3ME2xOE42OzZ7IN88US=> NYL1SphDW0GQR1XS
MZ2-MEL NHLaOIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M16wSGlEPTB;MUWuNlI2OSEQvF2= M3TVS3NCVkeHUh?=
COR-L88 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrVTWM2OD1zNj6wNFEzKM7:TR?= M3\kcXNCVkeHUh?=
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NCI-H719 NUjaW4R7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;ZTWM2OD1zNj65NVYyKM7:TR?= MVvTRW5ITVJ?
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SK-N-FI MkS1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXqXndVUUN3ME2xO{43QTF|IN88US=> MWLTRW5ITVJ?
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NCI-H1882 NW\y[Hh7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PnN2lEPTB;MUeuPVg{PCEQvF2= NGD3SFRUSU6JRWK=
A704 M1vOO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFr6W2hKSzVyPUG3Mlk6ODRizszN NGfmTIdUSU6JRWK=
L-428 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTF6LkCxOVEh|ryP MoL5V2FPT0WU
HCC1187 M{jKRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDZTWM2OD1zOD6wNVg4KM7:TR?= NEnxcmxUSU6JRWK=
NCI-H1581 NHfmUGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTF6LkC4OlYh|ryP MYHTRW5ITVJ?
BB65-RCC M1zuemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTF6LkSxOlIh|ryP NVPUTpA3W0GQR1XS
EM-2 NI[zOnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTF6LkW2O|Ih|ryP MnLSV2FPT0WU
Raji MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzDTWM2OD1zOT65OVY2KM7:TR?= NXnzR|U5W0GQR1XS
TE-1 MlvkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnuO5lQUUN3ME2yNE41OTB2IN88US=> M2\IUHNCVkeHUh?=
SW962 NV3NeWhTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjTbJFbUUN3ME2yNE41Ojl|IN88US=> NITsO5BUSU6JRWK=
MHH-NB-11 MnzBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XrWGlEPTB;MkCuOVUzOSEQvF2= MVTTRW5ITVJ?
no-10 M33xe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2X2cGlEPTB;MkGuNFI3PCEQvF2= NX7YOJd4W0GQR1XS
GDM-1 NHjyXXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXhOpBKSzVyPUKxMlk1OTRizszN MX;TRW5ITVJ?
KMS-12-PE NGriSHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7xTWM2OD1{Mj6yO|Qh|ryP NHPLbmlUSU6JRWK=
NCI-H510A M3GwR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTJ2LkGyO|gh|ryP NEnxc5FUSU6JRWK=
ES5 NWey[WRET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7DUGhKSzVyPUK0Mlc{PDlizszN MV7TRW5ITVJ?
JiyoyeP-2003 NXPmc5RLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXGzO5p1UUN3ME2yOk4zPzR{IN88US=> MUnTRW5ITVJ?
NMC-G1 NGXqPIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HHe2lEPTB;MkeuNVgzOiEQvF2= M{X4O3NCVkeHUh?=
NCI-H446 M1nXR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvTTWM2OD1{Nz60PVQ3KM7:TR?= MoXnV2FPT0WU
NB7 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTJ5LkmyNlkh|ryP M1\FfXNCVkeHUh?=
A388 M165NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPkPZhKSzVyPUK4MlAxPzRizszN M3q0e3NCVkeHUh?=
JVM-2 M3rTUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTJ6LkK4PVgh|ryP MV\TRW5ITVJ?
HT-144 NHmyc|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLOToVKSzVyPUK4MlY6KM7:TR?= MYjTRW5ITVJ?
NCI-H747 NITtPJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXYO2lKSzVyPUK4MlkyQTVizszN MoHTV2FPT0WU
NCI-H1650 Mm[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTJ7LkCxO|Yh|ryP M2fDN3NCVkeHUh?=
EB-3 M3\4Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlKzTWM2OD1{OT61N|A6KM7:TR?= MWLTRW5ITVJ?
KLE MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXmTWM2OD1{OT62NVkh|ryP M{W3e3NCVkeHUh?=
TK10 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PqNmlEPTB;M{CuNVI3KM7:TR?= M2HJ[HNCVkeHUh?=
COLO-668 NFz6dWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIX6dFBKSzVyPUOwMlc6OiEQvF2= NUn1[lNbW0GQR1XS
NCI-H23 MlHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHpTZlKSzVyPUOxMlExPjNizszN NVnwTINjW0GQR1XS
GOTO MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7FOmRoUUN3ME2zNU43ODh3IN88US=> M4XUd3NCVkeHUh?=
MSTO-211H M4K0fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUe3RXNyUUN3ME2zNU45Pjd6IN88US=> M33DfHNCVkeHUh?=
LB831-BLC M2OwdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTN{LkO4OFMh|ryP MmC0V2FPT0WU
SCH M{TafGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoSyTWM2OD1|Mj64OFg2KM7:TR?= NI\tRnBUSU6JRWK=
EHEB NVjSZWxUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml65TWM2OD1|ND6xNVk{KM7:TR?= Mnz1V2FPT0WU
U-266 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTN2LkK3PFEh|ryP NGDNXo5USU6JRWK=
EW-11 M1Tqbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2m3SmlEPTB;M{SuOFczPSEQvF2= NHnjd5dUSU6JRWK=
TE-9 MnTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nvfmlEPTB;M{euNFQxOSEQvF2= MWTTRW5ITVJ?
ES3 NEjvO5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTN5LkWwNFQh|ryP M3X5fnNCVkeHUh?=
NCI-H2141 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTSNWZKSzVyPUO4MlA5PDNizszN MXTTRW5ITVJ?
MPP-89 NEG5XW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\kWWtKSzVyPUSyMlA2QDZizszN M1L5UHNCVkeHUh?=
SK-MEL-2 NF;ndlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFm4SmpKSzVyPUSyMlY1ODVizszN NGrNSplUSU6JRWK=
LC-1F M2\MV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\HcG9KSzVyPUSzMlM3QDJizszN MVjTRW5ITVJ?
NH-12 M3TvNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjRbVVKSzVyPUSzMlk{PTlizszN MXLTRW5ITVJ?
RKO MmfKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfvRVRKSzVyPUS0MlEzPTJizszN NVTZ[2FVW0GQR1XS
KM-H2 NGrTPYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2j1TWlEPTB;NESuPVU4PyEQvF2= NYixTGx[W0GQR1XS
SK-UT-1 NF35Tm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorLTWM2OD12OT64PFI2KM7:TR?= NV35XlByW0GQR1XS

... Click to View More Cell Line Experimental Data

In vivo Consistent with the substantial and selective inhibition of VEGFR2 or PDGFR phosphorylation and signaling in vivo, Sunitinib (20-80 mg/kg/day) exhibits broad and potent dose-dependent anti-tumor activity against a variety of tumor xenograft models including HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435. Sunitinib dosing at 80 mg/kg/day for 21 days leads to complete tumor regression in six of eight mice, without tumor re-growing during a 110-day observation period after the end of treatment. Second round of treatment with Sunitinib remains efficacious against tumors that are not fully regressed during the first round of treatment. Sunitinib treatment results in significant decrease in tumor MVD, with ~40% reduction in SF763T glioma tumors. SU11248 treatment results in a complete inhibition of additional tumor growth of luciferase-expressing PC-3M xenografts, despite no reduction in tumor size. [2] Sunitinib treatment (20 mg/kg/day) dramatically suppresses the growth subcutaneous MV4;11 (FLT3-ITD) xenografts and prolongs survival in the FLT3-ITD bone marrow engraftment model. [3]

Protocol

Kinase Assay:[1]
+ Expand

Biochemical Tyrosine Kinase Assays:

IC50 values for Sunitinib against VEGFR2 (Flk-1) and PDGFRβ are determined using glutathione S-transferasefusion proteins containing the complete cytoplasmic domain of the RTK. Biochemical tyrosine kinase assays to quantitate the trans-phosphorylation activity of VEGFR2 (Flk-1) and PDGFRβ are performed in 96-well microtiter plates precoated (20 μg/well in PBS; incubated overnight at 4 °C) with the peptide substrate poly-Glu,Tyr (4:1). Excess protein binding sites are blocked with the addition of 1-5% (w/v) BSA in PBS. Purified GST-fusion proteins are produced in baculovirus-infected insect cells. GST-VEGFR2 and GST-PDGFRβ are then added to the microtiter wells in 2 × concentration kinase dilution buffer consisting of 100 mM HEPES, 50 mM NaCl, 40 μM NaVO4, and 0.02% (w/v) BSA. The final enzyme concentration for GST-VEGFR2 or GST-PDGFRβ is 50 ng/mL. Twenty-five μL of diluted Sunitinib are subsequently added to each reaction well to produce a range of inhibitor concentrations appropriate for each enzyme. The kinase reaction is initiated by the addition of different concentrations of ATP in a solution of MnCl2 so that the final ATP concentrations spanned the Km for the enzyme, and the final concentration of MnCl2 is 10 mM. The plates are incubated for 5-15 minutes at room temperature before stopping the reaction with the addition of EDTA. The plates are then washed three times with TBST. Rabbit polyclonal antiphosphotyrosine antisera are added to the wells at a 1:10,000 dilution in TBST containing 0.5% (w/v) BSA, 0.025% (w/v) nonfat dry milk, and 100 μM NaVO4 and incubated for 1 hour at 37 °C. The plates are then washed three times with TBST, followed by the addition of goat antirabbit antisera conjugated with horseradish peroxidase (1:10,000 dilution in TBST). The plates are incubated for 1 hour at 37 °C and then washed three times with TBST. The amount of phosphotyrosine in each well is quantitated after the addition of 2,2′-azino-di-[3-ethylbenzthiazoline sulfonate] as substrate.
Cell Research:[3]
+ Expand
  • Cell lines: RS4;11, MV4;11, and OC1-AML5
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 24 and 48 hours
  • Method: Cells are starved overnight in medium containing 0.1% FBS prior to addition of Sunitinib and FL (50 ng/mL; FLT3-WT cells only). Proliferation is measured after 48 hours of culture using the Alamar Blue assay or trypan blue cell viability assays. Apoptosis is measured 24 hours after Sunitinib addition by Western blotting to detect cleavage of poly (ADP-ribose) polymerase (PARP) or levels of caspase-3.
    (Only for Reference)
Animal Research:[2]
+ Expand
  • Animal Models: Female nu/nu mice implanted s.c. with HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435, and male nu/nu mice bearing luciferase-expressing PC-3M tumors
  • Formulation: Formulated as a carboxymethyl cellulose suspension or as a citrate buffered (pH 3.5) solution
  • Dosages: ~80 mg/kg
  • Administration: Orally once daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 15 mg/mL (28.16 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order:
4% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.
2mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 532.56
Formula

C22H27FN4O2.C4H6O5

CAS No. 341031-54-7
Storage powder
Synonyms N/A

Bio Calculators

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02761057 Recruiting Recurrent Renal Cell Carcinoma|Stage III Renal Cell Cancer|Stage IV Renal Cell Cancer|Type 1 Papillary Renal Cell Carcinoma|Type 2 Papillary Renal Cell Carcinoma National Cancer Institute (NCI) April 2016 Phase 2
NCT02779283 Recruiting Untreated Adult Acute Myeloid Leukemia OHSU Knight Cancer Institute|National Cancer Institute (NCI) December 2015 Phase 1
NCT02626754 Enrolling by invitation Renal Cell Carcinoma vghtpe user|Taipei Veterans General Hospital, Taiwan August 2015 Phase 2
NCT02465060 Recruiting Advanced Malignant Neoplasm|Lymphoma|Recurrent Plasma Cell Myeloma|Recurrent Solid Neoplasm|Refractory Malignant Neoplasm|Refractory Plasma Cell Myeloma National Cancer Institute (NCI) August 2015 Phase 2
NCT01835158 Active, not recruiting Clear Cell Renal Cell Carcinoma|Metastatic Renal Cell Cancer|Stage III Renal Cell Cancer|Stage IV Renal Cell Cancer National Cancer Institute (NCI) July 2013 Phase 2
NCT01740154 Terminated Fatigue|Recurrent Renal Cell Cancer|Stage IV Renal Cell Cancer Case Comprehensive Cancer Center|National Cancer Institute (NCI) September 2012 --

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    I was wondering that the compound is in its cis or trans form?

  • Answer:

    S1042 Sunitinib Malate is Z form.

  • Question 2:

    What is the difference between Sunitinib Malate(S1042) and Sunitinib(S7781)?

  • Answer:

    S1042 is the Malate salt form of Sunitinib. The biological activities of these two compounds are the same but the solubility of these two compounds in aqueous solvent are different.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID